| 规格 | 价格 | 库存 | 数量 |
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| 体外研究 (In Vitro) |
体外活性：Andarine 刺激 AR 介导的转录，达到 1 nM DHT 在 10 nM 浓度下观察到的转录水平的 93%。
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| 体内研究 (In Vivo) |
在前列腺和精囊中，GTx-007 (S-4) 只是部分激动剂，分别使完整动物的 33.8% 和 28.2% 恢复[2]。 GTx-007 显着提高 Wnt4 和 Wnt7a 子宫表达[2]。
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| 动物实验 |
Animal/Disease Models: Female C57BL/6J mice[2].
Doses: 0.5 mg/mouse. Route of Administration: Seven daily subcutaneous (sc) injections. Experimental Results: Resulted in a highly heterogeneous pattern of AR expression in all compartments, with a significant increase of AR-positive cells in the luminal epithelium compared to VC. Had approximately ten glands per uterine cross-section within an endometrium, with a compact stroma, consistent with overall endogenous steroid depletion. Did not detect any impact of GTx-007 on body weight. |
| 参考文献 |
[1]. Donghua Yin, et al. Pharmacodynamics of selective androgen receptor modulators. J Pharmacol Exp Ther. 2003 Mar;304(3):1334-40.
[2]. Ioannis Simitsidellis, et al. Selective androgen receptor modulators (SARMs) have specific impacts on the mouse uterus. J Endocrinol. 2019 Sep;242(3):227-239. |
| 分子式 |
C19H18F3N3O6
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| 分子量 |
441.36
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| CAS号 |
401900-40-1
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| 相关CAS号 |
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| SMILES |
FC(C1=C(C([H])=C([H])C(=C1[H])N([H])C([C@](C([H])([H])[H])(C([H])([H])OC1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)O[H])=O)[N+](=O)[O-])(F)F
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| 别名 |
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5%Propylene glycol:30mg/mL 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2657 mL | 11.3286 mL | 22.6572 mL | |
| 5 mM | 0.4531 mL | 2.2657 mL | 4.5314 mL | |
| 10 mM | 0.2266 mL | 1.1329 mL | 2.2657 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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